反应详情

温度

100 °C

To a solution of methyl 2-(5-hydroxy-1-methyl-1H-indazol-3-yl)-5-trityl-5H-pyrrolo[3,2-b]pyrazine-7-carboxylate (2.2 g, 3.9 mmol) in DMF (25 mL) was added K2CO3 (1.8 g, 12.8 mmol) and 1-chloro-4-methyl-4-nitropentane (1.0 g, 5.9 mmol), after the addition, the reaction mixture was heated to 100° C. with stirring for 4 hours. The reaction mixture was cooled to room temperature, H2O (25 mL) was added and product extracted with EtOAc (100 mL). The organic layer was washed with H2O (100 mL) and brine (100 mL), dried over Na2SO4 and concentrated under reduced pressure to give methyl 2-(1-methyl-5-(4-methyl-4-nitropentyloxy)-1H-indazol-3-yl)-5-trityl-5H-pyrrolo[3,2-b]pyrazine-7-carboxylate (1.8 g, 66.7%) as yellow solid. LCMS: (M+H)+=695.

1. additionafter the addition
2. temperatureThe reaction mixture was cooled to room temperature
3. extractionproduct extracted with EtOAc (100 mL)
4. washThe organic layer was washed with H2O (100 mL) and brine (100 mL)
5. dry with materialdried over Na2SO4
6. concentrationconcentrated under reduced pressure